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Assay Detail

CHEMBL920441

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of c-Kit by HTRF assay
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Mast/stem cell growth factor receptor Kit (CHEMBL1936)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor.
Dai Y, Hartandi K, Ji Z, Ahmed AA, Albert DH, Bauch JL, Bouska JJ, Bousquet PF, Cunha GA, Glaser KB, Harris CM, Hickman D, Guo J, Li J, Marcotte PA, Marsh KC, Moskey MD, Martin RL, Olson AM, Osterling DJ, Pease LJ, Soni NB, Stewart KD, Stoll VS, Tapang P, Reuter DR, Davidsen SK, Michaelides MR.
J Med Chem (2007) 50 : 1584 -1597
PubMed 17343372 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 7.23 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL374752 1 8.30
CHEMBL219887 1 8.00
CHEMBL374044 1 8.00
CHEMBL375670 1 7.89
CHEMBL373798 1 7.82
CHEMBL223360 LINIFANIB 3.0 1 7.80
CHEMBL374330 1 7.77
CHEMBL220057 1 7.77
CHEMBL220049 1 7.70
CHEMBL223790 1 7.58
CHEMBL219998 1 7.55
CHEMBL223528 1 7.50
CHEMBL223583 1 7.47
CHEMBL219727 1 7.41
CHEMBL424943 1 7.39
CHEMBL426004 1 7.38
CHEMBL376307 1 7.38
CHEMBL221053 1 7.38
CHEMBL219722 1 7.36
CHEMBL223304 1 7.32
CHEMBL223478 1 7.30
CHEMBL376245 1 7.28
CHEMBL219774 1 7.21
CHEMBL438653 1 7.19
CHEMBL222728 1 7.16
CHEMBL376077 1 7.07
CHEMBL222315 1 6.82
CHEMBL223361 1 6.82
CHEMBL373845 1 6.54
CHEMBL223572 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL374752 IC50 = 5.0 nM 8.30
CHEMBL219887 IC50 = 10.0 nM 8.00
CHEMBL374044 IC50 = 10.0 nM 8.00
CHEMBL375670 IC50 = 13.0 nM 7.89
CHEMBL373798 IC50 = 15.0 nM 7.82
CHEMBL223360 LINIFANIB IC50 = 16.0 nM 7.80
CHEMBL374330 IC50 = 17.0 nM 7.77
CHEMBL220057 IC50 = 17.0 nM 7.77
CHEMBL220049 IC50 = 20.0 nM 7.70
CHEMBL223790 IC50 = 26.0 nM 7.58
CHEMBL219998 IC50 = 28.0 nM 7.55
CHEMBL223528 IC50 = 32.0 nM 7.50
CHEMBL223583 IC50 = 34.0 nM 7.47
CHEMBL219727 IC50 = 39.0 nM 7.41
CHEMBL424943 IC50 = 41.0 nM 7.39
CHEMBL376307 IC50 = 42.0 nM 7.38
CHEMBL426004 IC50 = 42.0 nM 7.38
CHEMBL221053 IC50 = 42.0 nM 7.38
CHEMBL219722 IC50 = 44.0 nM 7.36
CHEMBL223304 IC50 = 48.0 nM 7.32
CHEMBL223478 IC50 = 50.0 nM 7.30
CHEMBL376245 IC50 = 53.0 nM 7.28
CHEMBL219774 IC50 = 61.0 nM 7.21
CHEMBL438653 IC50 = 65.0 nM 7.19
CHEMBL222728 IC50 = 69.0 nM 7.16
CHEMBL376077 IC50 = 86.0 nM 7.07
CHEMBL222315 IC50 = 152.0 nM 6.82
CHEMBL223361 IC50 = 150.0 nM 6.82
CHEMBL373845 IC50 = 290.0 nM 6.54
CHEMBL223572 IC50 = 400.0 nM 6.40
CHEMBL426887 IC50 = 850.0 nM 6.07
CHEMBL222778 IC50 = 7360.0 nM 5.13
CHEMBL220317 IC50 = 11200.0 nM 4.95
CHEMBL223185 IC50 > 12500.0 nM -